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Fulltext Revolutionizing Antiviral Therapeutics: Unveiling Innovative Approaches for Enhanced Drug Efficacy

Megantara S, Rusdin A, Budiman A, Shamsuddin S, Mohtar N, Muchtaridi M

Int J Nanomedicine, 2024;19:2889-2915.
PMID: 38525012 DOI: 10.2147/IJN.S447721

Since the beginning of the coronavirus pandemic in late 2019, viral infections have become one of the top three causes of mortality worldwide. Immunization and the use of immunomodulatory drugs are effective ways to prevent and treat viral infections. However, the primary therapy for managing viral infections remains antiviral and antiretroviral medication. Unfortunately, these drugs are often limited by physicochemical constraints such as low target selectivity and poor aqueous solubility. Although several modifications have been made to enhance the physicochemical characteristics and efficacy of these drugs, there are few published studies that summarize and compare these modifications. Our review systematically synthesized and discussed antiviral drug modification reports from publications indexed in Scopus, PubMed, and Google Scholar databases. We examined various approaches that were investigated to address physicochemical issues and increase activity, including liposomes, cocrystals, solid dispersions, salt modifications, and nanoparticle drug delivery systems. We were impressed by how well each strategy addressed physicochemical issues and improved antiviral activity. In conclusion, these modifications represent a promising way to improve the physicochemical characteristics, functionality, and effectiveness of antivirals in clinical therapy.

Matched MeSH terms: Pharmaceutical Preparations/chemistry
Fulltext Fruit pod extracts as a source of nutraceuticals and pharmaceuticals

Karim AA, Azlan A

Molecules, 2012 Oct 10;17(10):11931-46.
PMID: 23052712 DOI: 10.3390/molecules171011931

Fruit pods contain various beneficial compounds that have biological activities and can be used as a source of pharmaceutical and nutraceutical products. Although pods or pericarps are usually discarded when consuming the edible parts of fruits, they contain some compounds that exhibit biological activities after extraction. Most fruit pods included in this review contain polyphenolic components that can promote antioxidant effects on human health. Additionally, anti-inflammatory, antibacterial, antifungal and chemopreventive effects are associated with these fruit pod extracts. Besides polyphenolics, other compounds such as xanthones, carotenoids and saponins also exhibit health effects and can be potential sources of nutraceutical and pharmaceutical components. In this review, information on fruit pods or pericarp of Garcinia mangostana, Ceratonia siliqua, Moringa oleifera, Acacia nilotica, Sapindus rarak and Prosopis cineraria is presented and discussed with regard to their biological activity of the major compounds existing in them. The fruit pods of other ethno- botanical plants have also been reviewed. It can be concluded that although fruit pods are considered as being of no practical use and are often being thrown away, they nevertheless contain compounds that might be useful sources of nutraceutical and other pharmaceutical components.

Matched MeSH terms: Pharmaceutical Preparations/chemistry*
An insight into the role of experimental parameters in advanced oxidation process applied for pharmaceutical degradation

Qutob M, Alshehri S, Shakeel F, Alam P, Rafatullah M

Environ Sci Pollut Res Int, 2024 Apr;31(18):26452-26479.
PMID: 38546921 DOI: 10.1007/s11356-024-33040-3

The advanced oxidation process (AOP) is an efficient method to treat recalcitrance pollutants such as pharmaceutical compounds. The essential physicochemical factors in AOP experiments significantly influence the efficiency, speed, cost, and safety of byproducts of the treatment process. In this review, we collected recent articles that investigated the elimination of pharmaceutical compounds by various AOP systems in a water medium, and then we provide an overview of AOP systems, the formation mechanisms of active radicals or reactive oxygen species (ROS), and their detection methods. Then, we discussed the role of the main physicochemical parameters (pH, chemical interference, temperature, catalyst, pollutant concentration, and oxidant concentration) in a critical way. We gained insight into the most frequent scenarios for the proper and improper physicochemical parameters for the degradation of pharmaceutical compounds. Also, we mentioned the main factors that restrict the application of AOP systems in a commercial way. We demonstrated that a proper adjustment of AOP experimental parameters resulted in promoting the treatment performance, decreasing the treatment cost and the treatment operation time, increasing the safeness of the system products, and improving the reaction stoichiometric efficiency. The outcomes of this review will be beneficial for future AOP applicants to improve the pharmaceutical compound treatment by providing a deeper understanding of the role of the parameters. In addition, the proper application of physicochemical parameters in AOP systems acts to track the sustainable development goals (SDGs).

Matched MeSH terms: Pharmaceutical Preparations/chemistry
Recent advances in nanocellulose-based adsorbent for sustainable removal of pharmaceutical contaminants from water bodies: A review

Nordin AH, Yusoff AH, Husna SMN, Noor SFM, Norfarhana AS, Paiman SH, et al.

Int J Biol Macromol, 2024 Nov;280(Pt 2):135799.
PMID: 39307484 DOI: 10.1016/j.ijbiomac.2024.135799

The long-term presence of pharmaceutical pollution in water bodies has raised public awareness. Nanocellulose is often used in adsorption to remove pollutants from wastewater since it is an abundant, green and sustainable material. This paper offers an extensive overview of the recent works reporting the potential of nanocellulose-based adsorbents to treat pharmaceutical wastewater. This study distinguishes itself by not only summarizing recent research findings but also critically integrating discussions on the improvements in nanocellulose production and sorts of alterations based on the type of pharmaceutical contaminants. Commonly, charged, or hydrophobic characteristics are introduced onto nanocellulose surfaces to accelerate and enhance the removal of pharmaceutical compounds. Although adsorbents based on nanocellulose have considerable potential, several significant challenges impede their practical application, particularly concerning cost and scalability. Large-scale synthesis of nanocellulose is technically challenging and expensive, which prevents its widespread use in wastewater treatment plants. Continued innovation in this area could lead to breakthroughs in the practical application of nanocellulose as a superior adsorbent. The prospects of utilization of nanocellulose are explained, providing a sustainable way to address the existing restriction and maximize the application of the modified nanocellulose in the field of pharmaceutical pollutants removal.

Matched MeSH terms: Pharmaceutical Preparations/chemistry
Use of microwave in processing of drug delivery systems

Wong TW

Curr Drug Deliv, 2008 Apr;5(2):77-84.
PMID: 18393808

Microwave has received a widespread application in pharmaceuticals and food processing, microbial sterilization, biomedical therapy, scientific and biomedical analysis, as well as, drug synthesis. This paper reviews the basis of application of microwave to prepare pharmaceutical dosage forms such as agglomerates, gel beads, microspheres, nanomatrix, solid dispersion, tablets and film coat. The microwave could induce drying, polymeric crosslinkages as well as drug-polymer interaction, and modify the structure of drug crystallites via its effects of heating and/or electromagnetic field on the dosage forms. The use of microwave opens a new approach to control the physicochemical properties and drug delivery profiles of pharmaceutical dosage forms without the need for excessive heat, lengthy process or toxic reactants. Alternatively, the microwave can be utilized to process excipients prior to their use in the formulation of drug delivery systems. The intended release characteristics of drugs in dosage forms can be met through modifying the physicochemical properties of excipients using the microwave.

Matched MeSH terms: Pharmaceutical Preparations/chemistry*
From nanoemulsions to self-nanoemulsions, with recent advances in self-nanoemulsifying drug delivery systems (SNEDDS)

Rehman FU, Shah KU, Shah SU, Khan IU, Khan GM, Khan A

Expert Opin Drug Deliv, 2017 Nov;14(11):1325-1340.
PMID: 27485144 DOI: 10.1080/17425247.2016.1218462

INTRODUCTION: Lipid-based drug delivery systems (LBDDS) are the most promising technique to formulate the poorly water soluble drugs. Nanotechnology strongly influences the therapeutic performance of hydrophobic drugs and has become an essential approach in drug delivery research. Self-nanoemulsifying drug delivery systems (SNEDDS) are a vital strategy that combines benefits of LBDDS and nanotechnology. SNEDDS are now preferred to improve the formulation of drugs with poor aqueous solubility. Areas covered: The review in its first part shortly describes the LBDDS, nanoemulsions and clarifies the ambiguity between nanoemulsions and microemulsions. In the second part, the review discusses SNEDDS and elaborates on the current developments and modifications in this area without discussing their associated preparation techniques and excipient properties. Expert opinion: SNEDDS have exhibit the potential to increase the bioavailability of poorly water soluble drugs. The stability of SNEDDS is further increased by solidification. Controlled release and supersaturation can be achieved, and are associated with increased patient compliance and improved drug loads, respectively. Presence of biodegradable ingredients and ease of large-scale manufacturing combined with a lot of 'drug-targeting opportunities' give SNEDDS a clear distinction and prominence over other solubility enhancement techniques.

Matched MeSH terms: Pharmaceutical Preparations/chemistry
A comprehensive review on polyelectrolyte complexes

Meka VS, Sing MKG, Pichika MR, Nali SR, Kolapalli VRM, Kesharwani P

Drug Discov Today, 2017 11;22(11):1697-1706.
PMID: 28683256 DOI: 10.1016/j.drudis.2017.06.008

Global research on polyelectrolytes at a fundamental and applied level is intensifying because the advantages of sustainability are being accepted in academia and industrial research settings. During recent decades, polyelectrolytes became one of the most attractive subjects of scientific research owing to their great potential in the areas of advanced technologies. Polyelectrolytes are a type of polymer that have multitudinous ionizable functional groups. Ionized polyelectrolytes in solution can form a complex with oppositely charged polyelectrolytes - a polyelectrolyte complex (PEC). The present article provides a comprehensive review on PECs and their classification, theory and characterization, as well as a critical analysis of the current research.

Matched MeSH terms: Pharmaceutical Preparations/chemistry*
Enantioseparation of Selected Imidazole Drugs Using Dual Cyclodextrin-Modified Micellar Electrokinetic Chromatography

Ibrahim WAW, Wahib SMA, Hermawan D, Sanagi MM

Methods Mol Biol, 2019;1985:407-416.
PMID: 31069749 DOI: 10.1007/978-1-4939-9438-0_24

Particular attention has been paid to capillary electrophoresis as versatile and environmentally friendly approach for enantioseparations of a wide spectrum of compounds. Cyclodextrin-modified micellar electrokinetic chromatography (CD-MEKC) is a method of choice to provide effective separation toward hydrophobic and uncharged stereoisomers. The chiral discrimination of the solutes relies upon the partitioning between a given CD in the aqueous phase and micelles formed from a surfactant. Synergistic combinations of chiral selectors, surfactant, and modifier contribute to successful enantioseparations of the enantiomers. In this chapter, an application of CD-MEKC for the enantioseparation of selected imidazole drugs employing a dual CDs system is described.

Matched MeSH terms: Pharmaceutical Preparations/chemistry
Pharmacokinetic and Pharmacodynamic Features of Nanoemulsion Following Oral, Intravenous, Topical and Nasal Route

Choudhury H, Gorain B, Chatterjee B, Mandal UK, Sengupta P, Tekade RK

Curr Pharm Des, 2017;23(17):2504-2531.
PMID: 27908273 DOI: 10.2174/1381612822666161201143600

BACKGROUND: Most of the active pharmaceutical ingredients discovered recently in pharmaceutical field exhibits poor aqueous solubility that pose major problem in their oral administration. The oral administration of these drugs gets further complicated due to their short bioavailability, inconsistent absorption and inter/intra subject variability.
METHODS: Pharmaceutical emulsion holds a significant place as a primary choice of oral drug delivery system for lipophilic drugs used in pediatric and geriatric patients. Pharmacokinetic studies on nanoemulsion mediated drugs delivery approach indicates practical feasibility in regards to their clinical translation and commercialization.
RESULTS: This review article is to provide an updated understanding on pharmacokinetic and pharmacodynamic features of nanoemulsion delivered via oral, intravenous, topical and nasal route.
CONCLUSION: The article is of huge interest to formulation scientists working on range of lipophilic drug molecules intended to be administered through oral, intravenous, topical and nasal routes for vivid medical benefits.

Matched MeSH terms: Pharmaceutical Preparations/chemistry*
Fulltext Supersaturation Potential of Amorphous Active Pharmaceutical Ingredients after Long-Term Storage

Edueng K, Mahlin D, Gråsjö J, Nylander O, Thakrani M, Bergström CAS

Molecules, 2019 Jul 27;24(15).
PMID: 31357587 DOI: 10.3390/molecules24152731

This study explores the effect of physical aging and/or crystallization on the supersaturation potential and crystallization kinetics of amorphous active pharmaceutical ingredients (APIs). Spray-dried, fully amorphous indapamide, metolazone, glibenclamide, hydrocortisone, hydrochlorothiazide, ketoconazole, and sulfathiazole were used as model APIs. The parameters used to assess the supersaturation potential and crystallization kinetics were the maximum supersaturation concentration (Cmax,app), the area under the curve (AUC), and the crystallization rate constant (k). These were compared for freshly spray-dried and aged/crystallized samples. Aged samples were stored at 75% relative humidity for 168 days (6 months) or until they were completely crystallized, whichever came first. The solid-state changes were monitored with differential scanning calorimetry, Raman spectroscopy, and powder X-ray diffraction. Supersaturation potential and crystallization kinetics were investigated using a tenfold supersaturation ratio compared to the thermodynamic solubility using the µDISS Profiler. The physically aged indapamide and metolazone and the minimally crystallized glibenclamide and hydrocortisone did not show significant differences in their Cmax,app and AUC when compared to the freshly spray-dried samples. Ketoconazole, with a crystalline content of 23%, reduced its Cmax,app and AUC by 50%, with Cmax,app being the same as the crystalline solubility. The AUC of aged metolazone, one of the two compounds that remained completely amorphous after storage, significantly improved as the crystallization kinetics significantly decreased. Glibenclamide improved the most in its supersaturation potential from amorphization. The study also revealed that, besides solid-state crystallization during storage, crystallization during dissolution and its corresponding pathway may significantly compromise the supersaturation potential of fully amorphous APIs.

Matched MeSH terms: Pharmaceutical Preparations/chemistry*
Quality by Design Perspective for Designing Foam-based Formulation: Current State of Art

Kumar M, Kumar D, Singh S, Chopra S, Mahmood S, Bhatia A

Curr Pharm Des, 2024;30(6):410-419.
PMID: 38747045 DOI: 10.2174/0113816128289965240123074111

Foam-based delivery systems contain one or more active ingredients and dispersed solid or liquid components that transform into gaseous form when the valve is actuated. Foams are an attractive and effective delivery approach for medical, cosmetic, and pharmaceutical uses. The foams-based delivery systems are gaining attention due to ease of application as they allow direct application onto the affected area of skin without using any applicator or finger, hence increasing the compliance and satisfaction of the patients. In order to develop foam-based delivery systems with desired qualities, it is vital to understand which type of material and process parameters impact the quality features of foams and which methodologies may be utilized to investigate foams. For this purpose, Quality-by-Design (QbD) approach is used. It aids in achieving quality-based development during the development process by employing the QbD concept. The critical material attributes (CMAs) and critical process parameters (CPPs) were discovered through the first risk assessment to ensure the requisite critical quality attributes (CQAs). During the initial risk assessment, the high-risk CQAs were identified, which affect the foam characteristics. In this review, the authors discussed the various CMAs, CPPs, CQAs, and risk factors associated in order to develop an ideal foam-based formulation with desired characteristics.

Matched MeSH terms: Pharmaceutical Preparations/chemistry
A novel polymer inclusion membranes based optode for sensitive determination of Al³⁺ ions

Suah FB, Ahmad M, Heng LY

Spectrochim Acta A Mol Biomol Spectrosc, 2015 Jun 5;144:81-7.
PMID: 25748985 DOI: 10.1016/j.saa.2015.02.068

A novel approach for the determination of Al(3+) from aqueous samples was developed using an optode membrane produced by physical inclusion of Al(3+) selective reagent, which is morin into a plasticized poly(vinyl chloride). The inclusion of Triton X-100 was found to be valuable and useful for enhancing the sorption of Al(3+) ions from liquid phase into the membrane phase, thus increasing the intensity of optode's absorption. The optode showed a linear increase in the absorbance at λ(max)=425 nm over the concentration range of 1.85×10(-6)-1.1×10(-4) mol L(-1) (0.05-3 μg mL(-1)) of Al(3+) ions in aqueous solution after 5 min. The limit of detection was determined to be 1.04×10(-6) mol L(-1) (0.028 μg mL(-1)). The optode developed in the present work was easily prepared and found to be stable, has good mechanical strength, sensitive and reusable. In addition, the optode was tested for Al(3+) determination in lake water, river water and pharmaceutical samples, which the result was satisfactory.

Matched MeSH terms: Pharmaceutical Preparations/chemistry
Fulltext Ligand-based virtual screening using Bayesian inference network and reweighted fragments

Ahmed A, Abdo A, Salim N

ScientificWorldJournal, 2012;2012:410914.
PMID: 22623895 DOI: 10.1100/2012/410914

Many of the similarity-based virtual screening approaches assume that molecular fragments that are not related to the biological activity carry the same weight as the important ones. This was the reason that led to the use of Bayesian networks as an alternative to existing tools for similarity-based virtual screening. In our recent work, the retrieval performance of the Bayesian inference network (BIN) was observed to improve significantly when molecular fragments were reweighted using the relevance feedback information. In this paper, a set of active reference structures were used to reweight the fragments in the reference structure. In this approach, higher weights were assigned to those fragments that occur more frequently in the set of active reference structures while others were penalized. Simulated virtual screening experiments with MDL Drug Data Report datasets showed that the proposed approach significantly improved the retrieval effectiveness of ligand-based virtual screening, especially when the active molecules being sought had a high degree of structural heterogeneity.

Matched MeSH terms: Pharmaceutical Preparations/chemistry
Fulltext Solubility of drugs in aqueous polymeric solution: effect of ovalbumin on microencapsulation process

Aziz HA, Tan YT, Peh KK

AAPS PharmSciTech, 2012 Mar;13(1):35-45.
PMID: 22101965 DOI: 10.1208/s12249-011-9707-x

Microencapsulation of water-soluble drugs using coacervation-phase separation method is very challenging, as these drugs partitioned into the aqueous polymeric solution, resulting in poor drug entrapment. For evaluating the effect of ovalbumin on the microencapsulation of drugs with different solubility, pseudoephedrine HCl, verapamil HCl, propranolol HCl, paracetamol, and curcuminoid were used. In addition, drug mixtures comprising of paracetamol and pseudoephedrine HCl were also studied. The morphology, encapsulation efficiency, particle size, and in vitro release profile were investigated. The results showed that the solubility of the drug determined the ratio of ovalbumin to be used for successful microencapsulation. The optimum ratios of drug, ovalbumin, and gelatin for water-soluble (pseudoephedrine HCl, verapamil HCl, and propranolol HCl), sparingly water-soluble (paracetamol), and water-insoluble (curcuminoid) drugs were found to be 1:1:2, 2:3:5, and 1:3:4. As for the drug mixture, the optimum ratio of drug, ovalbumin, and gelatin was 2:3:5. Encapsulated particles prepared at the optimum ratios showed high yield, drug loading, entrapment efficiency, and sustained release profiles. The solubility of drug affected the particle size of the encapsulated particle. Highly soluble drugs resulted in smaller particle size. In conclusion, addition of ovalbumin circumvented the partitioning effect, leading to the successful microencapsulation of water-soluble drugs.

Matched MeSH terms: Pharmaceutical Preparations/chemistry*
Stability-indicating micellar electrokinetic chromatography method for the analysis of sumatriptan succinate in pharmaceutical formulations

Al Azzam KM, Saad B, Tat CY, Mat I, Aboul-Enein HY

J Pharm Biomed Anal, 2011 Dec 15;56(5):937-43.
PMID: 21873014 DOI: 10.1016/j.jpba.2011.08.007

A micellar electrokinetic chromatography method for the determination of sumatriptan succinate in pharmaceutical formulations was developed. The effects of several factors such as pH, surfactant and buffer concentration, applied voltage, capillary temperature, and injection time were investigated. Separation took about 5 min using phenobarbital as internal standard. The separation was carried out in reversed polarity mode at 20 °C, 26 kV and using hydrodynamic injection for 10s. Separation was achieved using a bare fused-silica capillary 50 μm×40 cm and background electrolyte of 25 mM sodium dihydrogen phosphate-adjusted with concentrated phosphoric acid to pH 2.2, containing 125 mM sodium dodecyl sulfate and detection was at 226 nm. The method was validated with respect to linearity, limits of detection and quantification, accuracy, precision and selectivity. The calibration curve was linear over the range of 100-2000 μg mL(-1). The relative standard deviations of intra-day and inter-day precision for migration time, peak area, corrected peak area, ratio of corrected peak area and ratio of peak area were less than 0.68, 3.48, 3.28, 2.97 and 2.83% and 2.01, 5.50, 4.46, 4.92 and 4.07%, respectively. The proposed method was successfully applied to the determinations of the analyte in tablet. Forced degradation studies were conducted by introducing a sample of sumatriptan succinate standard solution to different forced degradation conditions using neutral (water), basic (0.1 M NaOH), acidic (0.1 M HCl), oxidative (10% H(2)O(2)) and photolytic (exposure to UV light at 254 nm for 2 h). It is concluded that the stability-indicating method for sumatriptan succinate can be used for the analysis of the drug in various samples.

Matched MeSH terms: Pharmaceutical Preparations/chemistry*
Fulltext Stability assessment of injectable castor oil-based nano-sized emulsion containing cationic droplets stabilized by poloxamer-chitosan emulsifier films

Tamilvanan S, Kumar BA, Senthilkumar SR, Baskar R, Sekharan TR

AAPS PharmSciTech, 2010 Jun;11(2):904-9.
PMID: 20496017 DOI: 10.1208/s12249-010-9455-3

The objectives of the present work were to prepare castor oil-based nano-sized emulsion containing cationic droplets stabilized by poloxamer-chitosan emulgator film and to assess the kinetic stability of the prepared cationic emulsion after subjecting it to thermal processing and freeze-thaw cycling. Presence of cryoprotectants (5%, w/w, sucrose +5%, w/w, sorbitol) improved the stability of emulsions to droplet aggregation during freeze-thaw cycling. After storing the emulsion at 4 degrees C, 25 degrees C, and 37 degrees C over a period of up to 6 months, no significant change was noted in mean diameter of the dispersed oil droplets. However, the emulsion stored at the highest temperature did show a progressive decrease in the pH and zeta potential values, whereas the emulsion kept at the lowest temperatures did not. This indicates that at 37 degrees C, free fatty acids were formed from the castor oil, and consequently, the liberated free fatty acids were responsible for the reduction in the emulsion pH and zeta potential values. Thus, the injectable castor oil-based nano-sized emulsion could be useful for incorporating various active pharmaceutical ingredients that are in size from small molecular drugs to large macromolecules such as oligonucleotides.

Matched MeSH terms: Pharmaceutical Preparations/chemistry*
Simultaneous determination of ofloxacin and ornidazole in pharmaceutical preparations by capillary zone electrophoresis

See KL, Elbashir AA, Saad B, Ali AS, Aboul-Enein HY

Biomed Chromatogr, 2009 Dec;23(12):1283-90.
PMID: 19488980 DOI: 10.1002/bmc.1251

A simple, rapid and validated capillary electrophoretic method has been developed for the separation and determination of ofloxacin and ornidazole in pharmaceutical formulations with detection at 230 nm. Optimal conditions for the quantitative separations were investigated. Analysis times shorter than 4 min were obtained using a background electrolyte solution consisting of 25 mmol/L phosphoric acid adjusted with 1 M Tris buffer to pH 8.5, with hydrodynamic injection of 5 s and 20 kV separation voltage. The validation criteria for accuracy, precision, linearity and limits of detection and quantitation were examined and discussed. An excellent linearity was obtained in concentration range 25-250 microg/mL. The detection limits for ofloxacin and ornidazole were 1.03 +/- 0.11 and 1.80 +/- 0.06 microg/mL, respectively. The proposed method has been applied for the analysis of ofloxacin and ornidazole both individually and in a combined dosage tablet formulation. The proposed validated method showed recoveries between 96.16 and 105.23% of the nominal contents.

Matched MeSH terms: Pharmaceutical Preparations/chemistry*
In Situ Gelling Ophthalmic Drug Delivery System: An Overview and Its Applications

Sheshala R, Kok YY, Ng JM, Thakur RR, Dua K

Recent Pat Drug Deliv Formul, 2015;9(3):237-48.
PMID: 26205681

Ophthalmic drug delivery system is very interesting and challenging due to the normal physiologically factor of eyes which reduces the bioavailability of ocular products. The development of new ophthalmic dosage forms for existing drugs to improve efficacy and bioavailability, patient compliance and convenience has become one of the main trend in the pharmaceuticals industry. The present review encompasses various conventional and novel ocular drug delivery systems, methods of preparation, characterization and recent research in this area. Furthermore, the information on various commercially available in situ gel preparations and the existing patents of in situ drug delivery systems i.e. in situ gel formation of pectin, in situ gel for therapeutic use, medical uses of in situ formed gels and in situ gelling systems as sustained delivery for front of eye are also covered in this review.

Matched MeSH terms: Pharmaceutical Preparations/chemistry
Nanospray Drying Technology: Existing Limitations and Future Challenges

Wui WT

Recent Pat Drug Deliv Formul, 2015;9(3):185-6.
PMID: 25966873
Matched MeSH terms: Pharmaceutical Preparations/chemistry*
Investigation on Secondary Structure Alterations of Protein Drugs as an Indicator of Their Biological Activity Upon Thermal Exposure

Zeeshan F, Tabbassum M, Kesharwani P

Protein J, 2019 10;38(5):551-564.
PMID: 31054037 DOI: 10.1007/s10930-019-09837-4

Protein drugs are important therapeutic agents however; they may degrade during formulation processing. The objective of this study was to investigate the correlation between secondary structure alterations and the retentions of biological activity of protein upon the application of thermal stress. Catalase, horseradish peroxidase and α- chymotrypsin were employed as model proteins. Each protein was heated in a solid and solution state at a temperature of 70 °C for 1 h. Attenuated total reflectance Fourier transform infrared spectroscopy, size-exclusion chromatography and biological activity assay were performed. Results showed that heat-exposure of protein solids at 70 °C caused minimum changes in secondary structure and biological activity was almost retained. However, thermal exposure of protein aqueous solution induced significant changes in the secondary structure indicated by area overlap values and caused considerable reduction in the biological activity. The changes in secondary structures were found to be in full alignment with the loss of biological activity for both protein solids as well as aqueous solutions. Catalase lost entire biological activity upon heating in the solution state. In conclusion, the findings of the present study indicate a direct correlation between protein secondary structure alterations and the retention of biological activity which can be taken into account during the development and delivery of protein drugs formulations.

Matched MeSH terms: Pharmaceutical Preparations/chemistry

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